PHA 767491 hydrochloride

Catalog # Availability Size / Price Qty
3140/10
3140/50
PHA 767491 hydrochloride | CAS No. 942425-68-5 | Cyclin-dependent Kinase Inhibitors
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Description: MK2 inhibitor; also cdk inhibitor; potently inhibits cdk9

Chemical Name: 1,5,6,7-Tetrahydro-2-(4-pyridinyl)-4H-pyrrolo[3,2-c]pyridin-4-one hydrochloride

Purity: ≥99%

Product Details
Citations (5)
Reviews

Biological Activity

ATP-competitive cyclin-dependent kinase (cdk) inhibitor (reported IC50 values are 0.034 - 0.75, 0.24 - 1.2, 0.25 - 1.1 and 0.46 - 1 μM for cdk9, cdk2, cdk1 and cdk5, respectively). Also inhibits mitogen-activated protein kinase-activated protein kinase-2 (MK2; IC50 = 171 nM). Prevents initiation of DNA replication. Inhibits cell proliferation in a variety of human cell lines and induces apoptosis in a p53-independent manner in vivo.

Technical Data

M.Wt:
249.7
Formula:
C12H11N3O.HCl
Solubility:
Soluble to 100 mM in water and to 100 mM in DMSO
Purity:
≥99%
Storage:
Desiccate at RT
CAS No:
942425-68-5

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2).
    Anderson et al.
    J.Med.Chem., 2007;50:2647
  2. Stopping replication, at the beginning.
    Jackson
    Nature Chem.Biol., 2008;4:331
  3. A cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumour activity.
    Montagnoli et al.
    Nature Chem.Biol., 2008;4:357
  4. How selective are pharmacological inhibitors of cell-cycle-regulating cyclin-dependent kinases?
    Jorda et al.
    J.Med.Chem., 2018;61:9105

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Citations for PHA 767491 hydrochloride

The citations listed below are publications that use Tocris products. Selected citations for PHA 767491 hydrochloride include:

5 Citations: Showing 1 - 5

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